反应详情

温度

100 °C

To a 40 mL scintillation vial was charged 3-quinoline boronic acid (0.73 mmol, 127 mg), K3PO4 (1.46 mmol, 310 mg) and PdCl2(dppf).CH2Cl2 (0.049 mmol, 40 mg). To this mixture was added a solution of ethyl 2-(4-(7-(bis((2-(trimethylsilyl)ethoxy)methyl)amino)-3-iodopyrazolo[1,5-a]pyrimidin-5-yl)cyclohexyl)acetate (335 mg, 0.49 mmol) in dioxane (9 mL). To this suspension was added distilled H2O (1 mL). The resulting solution was stirred at 100° C. for 18 hours. The reaction was concentrated in vacuo and then purified via silica gel chromatography (0% to 60% ethyl acetate in hexanes gradient) to yield ethyl 2-(4-(7-(bis((2-(trimethylsilyl)ethoxy)methyl)amino)-3-(quinolin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)cyclohexyl)acetate (198 mg, 287 μmol, 59% yield) as yellow oil.

1. additionTo this suspension was added
2. distillationdistilled H2O (1 mL)
3. concentrationThe reaction was concentrated in vacuo
4. custompurified via silica gel chromatography (0% to 60% ethyl acetate in hexanes gradient)